Josamycin

Chemical name

3-Ацетат-4В-(3-метилбута ноат)лейкомицин V

Gross

C42-H69-N-O15

Characteristics

It is soluble in methanol and ethanol-soluble on the air and very little in the water. Producyruetsa aktinomicetami Streptomyces narbonensis var. josamyceticus.

Of drugs

Drugs, the Sun. Reversible associated with the 50S subjedinica ribosom inhibits protein synthesis and distribution of microbial cells (bakteriostaticeski effect). When creating stable inflammation high concentrations has a bactericidal effect. It has a wide range of activity, including gram (Staphylococcus spp. , Producyrute not producyrute penitsillinazou, Streptococcus spp. Bacillus anthracis, Corynebacterium diphtheriae) and gram (Neisseria gonorrhoeae, N. meningitidis, some Shigella species, Haemophilus influenzae, Bordetella pertussis) bacteria, microorganisms Wärmetauscher (Legionella spp, Mycoplasma spp. , Chlamydia spp. , Ureaplasma urealyticum), and some anaeroba (Peptococcus, Peptostreptococcus, Clostridium perfringens, Bacteroides fragillis). Light affects the enterobacteria, because little change natural bacterial flora stomach. Effective resistance to the introduction Eritromitinu.pri Female pregnant mice and rats during organogeneza dose of 3 g / kg increased mortality and cause delay in the fruit without signs tertogennogo Actia.posle intake of rapidly and completely absorbed from the digestive tract, eating does not affect the bioavailability. C_max achieved through 0.5-2 h in a single dose of 400 mg, 0.33 mg / l, 500 mg-0,67-0,71 mg / l, 1000 mg, 2.4 mg / l, 1250 mg, 2.08 1.13 mg / l, 2000 mg, 5.79 +2.47 mg / O Associated with the plasma protein 15%. Well soluble in fats and little ionize under normal pH values of the blood and tissue fluids, well permeates through gistogematicalkie barriers to the various organs and tissues. The distribution 300.56 litres. The largest concentrations are in the respiratory system, including the lungs, sputum (maximum level in sputum achieved within 1 h and exceeds the concentration in plasma at 8-9 times), mindalinah, adenoidah, ekssoudate middle ear, okolonosovykh secret ingredient, slezna fluid saliva, desnah, bones, prostate and port glands. Concentration in sputum. Hardly enters spinnomozgovu liquid that passes through the placenta and secretiruetsa in breast milk. Biotransformiroetsa in the liver with the formation of three inactive metabolites : 14-gidroksidjozamitsin, and gidroksidjozamitsin деизовалерилджозамиц ин. T_1/2 - 0,9-2 hours (an average of 1.5 h), increased by cirrhosis of the liver. Excreted mainly jelchew and urine (less than 20%).

Indications

Инфекционно-воспалит��льные acute respiratory diseases and Lor-organov : tonsillitis, pharyngitis, laringit, sinusit average otitis, and tonzillit paratonzillit, bronchitis, pneumonia, bronhoektatical disease; dental infections (gingivit, parodontit); infections of skin and soft tissues (fat, piodermia, furunkoulez, anthrax, rojistoe inflammation, limphangit, lymphadenitis, venerica limfogranulema); infection urinary tract (prostatitis, Baby); diphtheria, scarlet fever, whooping cough, gonorrhoea, syphilis, chlamydia, ornitos, dysentery, dakriotistit, blefarit.

Restrictions on the use of

Pregnancy, breast feeding, old age.

Pregnancy and lactation

Perhaps during pregnancy, if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Гиперчувствительност ь (incl. to makrolidam etc.), heavy of the liver.

Side-Effects

For part of the intestine : oblojennosti language, anorexia, nausea, heartburn, vomiting, bloating, pain in the abdomen, diarrhoea, melena, a breach of the liver, the increase in the liver transaminaz (AST, ALT), holetsaticeski hepatitis, psevdomembranosny Kolit.prochie : swelling feet, a violation hearing, goiter, candidiasis, allergic reactions (urticaria, rash), a very rare, fever, general malaise.

Specific guidance

Suspension should be used within four weeks after opening bottle.

Patient interaction

Wrinkles down theofillina (increasing side effects), and astemizola terfenadina (increased risk of jeludockovh arrhythmias. Potenziruet vazokonstrictornoe the alkaloids LPV. Ters effect of hormonal contraceptives. Decreases effective microbicides antibiotics and linkomitina (mutually). It increases the concentration of cyclosporine (risk of nefrotoksicnosti) midazolama, triazolama, digoxin and bromokriptina plasma. Stops metabolism dizopiramida, diversion (increases T_1/2) carbamazepina.

Overdosing

Symptoms : Symptoms increased by Effectov.lechenie : symptomatic therapy.

Precautions

In order to prevent the emergence of resistant strains to a minimum duration of the course (with streptococcal infections of not less than 10 days), not to increase or double the dose if the admission was allowed. During a therapy ECG monitoring (particularly in patients while receiving digoxin), the control functions of the kidneys and liver. When treating diabetes, it should be borne in mind that 5 ml suspension containing 3.25 g glucose. People older designate smaller doses and treatments under the supervision of a physician.

Dosing and Administration

Inside, between meals. Pills with liquid, squeezed small amounts of water. Adults and children over 14 years of age, 1-2 g / day 2-3 reception. Treatment ordinary and teens ball on the 500 mg twice a day over a period of two to four weeks, then 500 mg once a day for 8 weeks. Children preferably in the form of suspension 6-14 years (weight over 21 kg) dose of 30 to 45 ml / day, 1-6 years old (weight 10-21 kg) 15-30 ml / day, 3 months to 1 year (weight 5,5-10 kg) Seven ml / day, divided into three reception.

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